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目的制备芒果苷(mangiferin,MGF)自微乳给药系统(SMEDDS),并对其进行药动学研究。方法评价系统自微乳化速度,激光散射仪测定乳化后形成微乳粒径的大小及分布情况;以PBS6.8缓冲液为释放介质,考察MGF-SMEDDS的体外释放行为;采用HPLC法测定大鼠血浆药物浓度,考察MGF-SMEDDS的体内吸收情况。结果体系在1min内可乳化完全,乳化后粒径在20nm左右;MGF-SMEDDS在120min的累积释放率可达80%以上;大鼠体内药动学研究结果表明,MGF-SMEDDS达峰时间为0.43h,是MGF的1/7;最大血药浓度为0.93mg/L,是MGF的2.16倍。结论自微乳给药系统可以显著提高MGF的体外释放,改善其药动学性质。
Objective To prepare mangiferin (MGF) self-microemulsion delivery system (SMEDDS) and study its pharmacokinetics. Methods The self-microemulsification rate of the system was evaluated. The size and distribution of microemulsion size after emulsification were determined by laser light scattering instrument. The release behavior of MGF-SMEDDS in vitro was evaluated by PBS6.8 buffer. Plasma drug concentrations were examined for in vivo absorption of MGF-SMEDDS. The results showed that the system could be emulsified completely within 1 min and the particle size was about 20 nm after emulsification. The cumulative release rate of MGF-SMEDDS reached more than 80% at 120 min. The pharmacokinetics results of MGF-SMEDDS showed that the peak time of MGF-SMEDDS reached 0.43 h, which is 1/7 of MGF. The maximum plasma concentration is 0.93 mg / L, which is 2.16 times that of MGF. Conclusion Self-microemulsion delivery system can significantly improve the in vitro release of MGF and improve its pharmacokinetics.